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PDE4-IN-6
MCE 国际站：PDE4-IN-6
产品活性：PDE4-IN-6 是一种有效、安全且具有中等选择性的 PDE4 抑制剂，对 PDE4B 和 PDE4D 的 IC50 分别为 0.125和0.43 µM。PDE4-IN-6 可下调 TNF-α 和 IL-6 的表达水平。PDE4-IN-6 具有强大的免疫调节活性，具有抗类风湿性关节炎的研究潜力。还具有抗炎、抗关节炎的作用。
研究领域：Metabolic Enzyme/Protease
作用靶点：Phosphodiesterase (PDE)
In Vitro: PDE4-IN-6 (compound 5f) (0.1-10 µM; 1 hour) has concentration-dependent inhibition on TNF-α in Raw 264.7 cells, with 42.3, 49.6, 57.2 and 68.7% inhibition at concentration of 0.3, 1, 3 and 10 µM.
In Vivo: PDE4-IN-6 (10 and 30 mg/kg; i.p.; daily from day 11 until day 20) can improve body weight and reduce paw swelling, also ameliorate joint space narrowing, cartilage degeneration and joint structural deformity in AIA rats at dosing 30 mg/kg.
PDE4-IN-6 (1-100 μM; incubated 4 days, 3 days or 4 hours) does not induce teratogenicity, hepatotoxicity and cardiac toxicity in zebrafish embryos.
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文献和实验Generation of PDE4 Knockout Mice by Gene Targeting
by homologous recombination in mouse ES cells in vitro has been established as a powerful means of altering specific loci in the mouse genome. As a result, gene function can be studied in vivo. By applying this technology, targeted disruption of PDE4 alleles
Renaturation of the Catalytic Domain of PDE4A Expressed in Escherichia coli as Inclusion Bodies
bodies and optimal conditions have to be determined empirically for any given protein. Here, we describe a simple and efficient refolding protocol for the catalytic domain of type 4 cyclic nucleotide phosphodiesterases (PDE4s). This method
Recently, it has been shown that enzymes of the cyclic adenosine monophosphate (cAMP)-specific phosphodiesterase (PDE) family 4 can be directly phosphorylated by extracellular signal-regulated kinase 2 (ERK2). Phosphorylation of PDE4s by ERK
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